Home Epigenetics Epigenetic Reader Domain inhibitor - Histone Methyltransferase inhibitor - PROTAC inhibitor UNC6852

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UNC6852 Epigenetic Reader Domain inhibitor

UNC6852 is a selective degrader that targets polycomb repressive complex 2 (PRC2) with IC50 of 247 nM for EED. This compound is based on PROTAC and contains an EED226-derived ligand and a ligand for VHL.

UNC6852 Epigenetic Reader Domain inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 832.97

Purity & Quality Control

Batch: S965901 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.83%
99.83

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Mechanism of Action

Targets
EED [1]
(Cell-free assay)
247 nM

In vitro
In vitro

UNC6852 contains an EED226-derived ligand and a ligand for VHL which bind to the WD40 aromatic cage of EED and CRL2VHL, respectively, to induce proteasomal degradation of PRC2 components, EED, EZH2, and SUZ12. Degradation of PRC2 with this compound blocks the histone methyltransferase activity of EZH2, decreasing H3K27me3 levels in HeLa cells and diffuse large B cell lymphoma (DLBCL) cells containing EZH2 gain-of-function mutations. This chemical degrades both wild-type and mutant EZH2, and additionally displays anti-proliferative effects in this cancer model system.[1]
Cell Research Cell lines Hela cells
Concentrations 0.1 μM, 0.5 μM, 1 μM, 3 μM, 5 μM, 10 μM, 20 μM, 30 μM
Incubation Time 2 h, 4 h, 8 h, 10 h, 16 h, 20 h, 24 h, 48 h, 72 h
Method

Jess Protein Simple is used according to product guideline instructions. HeLa cells are treated with bivalent degraders UNC6852 at 5 μM for 4 hrs, 24 hrs, and 48 hrs, and cell lysates are generated using a modified RIPA buffer. Cell lysates are used at 1 mg/mL. The primary antibodies used are: anti-EED, anti-EZH2. The secondary antibodies used are: anti-sheep HRP secondary antibody, anti-rabbit secondary IR antibody.

References
  • https://pubmed.ncbi.nlm.nih.gov/31831267/

Chemical Information

Molecular Weight 832.97 Formula
C43H48N10O6S
CAS No. 2688842-08-0 SDF --
Synonyms N/A
Smiles CC1=C(SC=N1)C2=CC=C(CNC(=O)C3CC(O)CN3C(=O)C(NC(=O)CCCNC(=O)C4=CC=C(C=C4)C5=CN=C(NCC6=CC=CO6)[N]7C=NN=C57)C(C)(C)C)C=C2

Storage and Stability

Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (120.05 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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